π‘ PROTON PUMP INHIBITORS (PPIs)
π§ What Are PPIs?
PPIs are the most potent acid-suppressing drugs available.
They block the final step in acid production: the proton pump (H+, K+-ATPase) in parietal cells.
They suppress ALL gastric acidβstimulated (meal/acid/histamine-induced) and basal/nighttime.
π PROTOTYPE: Omeprazole (Prilosec)
β Mechanism of Action
Irreversibly binds to the H+, K+-ATPase (proton pump).
Prevents HCl from being secreted into the stomach lumen.
Suppresses acid production from histamine, acetylcholine, and gastrin.
π¬ Pharmacokinetics
Property | Details |
|---|---|
Absorption | Well absorbed orally |
Binding | 95% protein bound |
Metabolism | Liver (CYP2C19 β watch for drug interactions!) |
Excretion | Mostly urine (75%), some feces |
Half-life | 1β1.5 hrs |
Duration | Acid suppression lasts 72+ hours |
Onset | Acid suppression in 2 hrs |
Persistence | Effects last 48β72 hrs after stopping (until new pumps are made) |
π USE
PUD (duodenal & gastric ulcers)
Faster healing than H2RAs: ~2 weeks vs. 4 weeks
GERD (esp. erosive esophagitis)
Relief in 1β2 weeks
Esophagitis heals in ~8 weeks
Zollinger-Ellison syndrome
H. pylori ulcers β used in triple therapy (PPI + 2β3 antibiotics + bismuth)
π§ββ SPECIAL POPULATIONS
π΅ Older Adults
Tolerate PPIs well
Preferred for GERD (need stronger acid suppression)
Caution with long-term use (>1 year):
β hip fracture risk (β Ca2+ absorption from achlorhydria)
β dementia risk in some
Use lowest effective dose for shortest time
π€° Pregnancy & Breastfeeding
Drug | Pregnancy Use | Notes |
|---|---|---|
Omeprazole | β Contraindicated | Linked to congenital cardiac defects |
Lansoprazole | β Safe | Can use in pregnancy |
Pantoprazole | β Safe | Preferred in pregnancy |
Rabeprazole | β Safe | Also tolerated well |
OK during lactation β used successfully in neonates
π° Renal & Liver Impairment
No dose adjustments typically needed
Caution: Bioavailability β in liver disease (β first-pass metabolism)
Can β LFTs transiently
π₯ Critically Ill
Best choice for stress ulcer prophylaxis
Available IV (esomeprazole, pantoprazole)
Very effective and well tolerated
π¨ ADVERSE EFFECTS
Most Common:
Nausea
Diarrhea
Headache
Abdominal pain
Long-Term/High-Dose Risks:
Hypocalcemia β fractures
Hypomagnesemia β muscle cramps, seizures
β Vitamin B12 absorption β fatigue, weakness, neuro symptoms
Watch for:
Chvostek & Trousseau signs (low calcium)
Hyperreflexia/seizures (low magnesium)
β CONTRAINDICATIONS
Hypersensitivity to omeprazole
Pregnancy (omeprazole specifically)
Caution: CYP2C19 genetic variants β β metabolism β β drug levels/toxicity
π DRUG INTERACTIONS (Important!!)
πΌ Increases levels of:
Warfarin
Phenytoin
Benzodiazepines (e.g., diazepam)
Clarithromycin (β omeprazole effects)
β¬ Decreases effectiveness of:
Clopidogrel (β anti-platelet effect β β cardiac patients)
𧬠Metabolized by CYP450βespecially CYP2C19
β omeprazole and esomeprazole = highest interaction risk
π ADMINISTRATION GUIDELINES
Take BEFORE meals (empty stomach)
Do NOT chew or crush delayed-release capsules/tablets
Two 20-mg β One 40-mg β too much sodium bicarbonate in 2x20 mg doses!
For patients with NG tubes or swallowing issues:
Sprinkle granules on applesauce (e.g., dexlansoprazole, lansoprazole)
Mix with water (esomeprazole)
Pantoprazole IV:
Administer over 15 minutes
Use in-line filter
Flush line with dextrose, saline, or lactated Ringer's
π§ͺ THERAPEUTIC EFFECTS
Decrease in:
Epigastric pain
Heartburn
Ulcer healing in 2β8 weeks
Monitor pH, symptom relief, and endoscopy/radiology if needed
π§ ADVERSE EFFECT MONITORING
GI: Nausea, diarrhea, vomiting
CNS: Headache, dizziness
Labs:
Magnesium
Calcium
B12
Watch for:
Muscle cramps, hyperreflexia, seizures (low Mg)
Fatigue, neuropathy, tongue soreness (low B12)
Bone fractures (esp. hip/wrist/spine)
π©π½ββοΈ PATIENT TEACHING (Based on Box 37.1 & Clinical Case)
β Proper Administration
Take before eating
Swallow capsules/tablets whole
Donβt use antacids within 1 hour
Donβt take OTC PPI >14 days without provider
Donβt substitute two 20 mg for one 40 mg
β Dietary Guidelines
AVOID foods that trigger acid:
Spicy, fatty, fried foods
Chocolate
Coffee
Alcohol
Citrus/acidic juices
Include:
Bland foods (bananas, rice, toast)
Lean protein
Low-fat dairy (if tolerated)
Calcium/magnesium-rich foods to help counter deficiencies
β Lifestyle Modifications
Elevate head of bed
Eat small meals
Avoid lying down 1β2 hrs after eating
Stop smoking
Prevent constipation
π§ OTHER PPIs β What Makes Them Different?
Drug | Key Notes |
|---|---|
Dexlansoprazole | OK to open capsules, sprinkle on applesauce. NG use approved. |
Esomeprazole | Available IV. Less drug interaction than omeprazole. |
Lansoprazole | Can sprinkle/mix granules with 30 mL water, acidic food, or applesauce. Caution in liver impairment. |
Pantoprazole | Lowest interaction risk. IV form. Can give with or without food. |
Rabeprazole | Metabolized more by CYP3A4 β fewer drug interactions. Good in liver disease. |
π CLINICAL TEACHING PLAN: MS. CARPENTER
π What to Teach
Take omeprazole 40 mg once daily before food
Donβt crush/chew β swallow whole
Report abdominal pain, black stools, signs of bleeding
Lifestyle changes (see above)
Continue antacid & sucralfate as directed (spaced 1β2 hours apart)
π₯ Nutritional Teaching
Avoid:
Fried, fatty, spicy foods
Chocolate, alcohol, caffeine
Tomato-based sauces, citrus
Include:
Bland, low-acid foods
Bone health foods: leafy greens, almonds, dairy
Iron-rich & B12-rich foods: lean meat, spinach, eggs
β QUICK KEY TAKEAWAYS: PPIs
PPIs = strongest acid reducers available
Omeprazole = prototype, but high risk for drug interactions
Take BEFORE meals, donβt crush tablets
Used for PUD, GERD, ZollingerβEllison, H. pylori ulcers
Long-term use: watch for fractures, hypocalcemia, B12 & magnesium deficiency
Preferred over H2RAs for severe/erosive GERD
Pantoprazole = safest PPI for polypharmacy patients